Synthesis of Biotin-Labelled Dexamethasone Derivatives. Novel Hormone-Affinity Probes

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Abstract
A new, general methodology for ‘sandwich’ affinity chromatography of steroid hormone receptors is proposed, the part purification of the human spleen tumor glucocorticoid receptor is quoted as an illustration. 9‐Fluoro‐16α‐methyl‐11β,17‐dihydroxy‐1,4‐androstadiene‐3‐one‐17β‐carboxylic acid was coupled to biotin using pentamethylenediamine (BioDex 1) as a spacer. The bifunctional derivative binds to glucocorticoid receptors and avidin‐Sepharose and efficiently protects the glucocorticoid receptor against inactivation when previously added during homogenisation. We have standardized the capacity and optimum conditions for elution of receptor ‐ BioDex‐1 complexes which are bound to avidin‐Sepharose. Receptor purification of several thousandfold can be obtained with good yield.